An efficient and cost-effective synthesis of 2-phenyl-3-aminopyridine

被引:43
作者
Caron, S [1 ]
Massett, SS [1 ]
Bogle, DE [1 ]
Castaldi, MJ [1 ]
Braish, TF [1 ]
机构
[1] Pfizer Inc, Global Res & Dev, Chem Res & Dev, Groton, CT 06340 USA
关键词
D O I
10.1021/op000227e
中图分类号
O69 [应用化学];
学科分类号
081704 ;
摘要
The synthesis of 2-phenyl-3-aminopyridine, a key intermediate in the preparation of 2-phenyl-3-aminopiperidine, from 2-chloro-3-aminopyridine is described using an imine as a protecting group for an aminopyridine, The in situ protection of 2-chloro-3-aminopyridine with benzaldehyde followed by Suzuki coupling with phenylboronic acid and subsequent acid hydrolysis provided the titled compound in a single, high-yielding step from inexpensive and commercially available starting materials.
引用
收藏
页码:254 / 256
页数:3
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